Drug intelligence / Profile preview

adavosertib + itraconazole

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

**Adavosertib + itraconazole** is an experimental combination involving two drugs: adavosertib, a selective small molecule inhibitor of the WEE1 kinase, and itraconazole, an antifungal agent known for potent inhibition of the cytochrome P450 enzyme CYP3A4. This combination is studied primarily to evaluate the pharmacokinetic (PK) effects and drug-drug interactions in patients with advanced solid tumors. Adavosertib disrupts the G2/M cell cycle checkpoint, augmenting DNA damage-induced cell death in cancers, while itraconazole is used in this setting to alter adavosertib metabolism by impeding its breakdown via CYP3A4, increasing its bioavailability. There are no unique brand names or commercial formulations for this combination, and it is not an approved regimen but rather used in clinical PK interaction studies[1][2].

Other names
adavosertib + itraconazole
02

Targets

CYP3A4 (Cytochrome P450 3A4)WEE1 (WEE1 G2 checkpoint kinase)

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